Drug intelligence / Profile preview

BI 691751 + itraconazole

Development stage
Discontinued
Lead developer
Boehringer
Modality
Small Molecules
Administration
Oral
01

Overview

BI 691751 + itraconazole is an investigational combination used in clinical pharmacokinetic studies to assess drug-drug interaction. BI 691751 is a **small molecule inhibitor of Leukotriene A-4 hydrolase (LTA4H)**, developed primarily for cardiovascular indications such as atherosclerosis. Itraconazole is a well-established antifungal agent and a potent inhibitor of **CYP3A4** and **P-glycoprotein (P-gp)**, commonly used experimentally to evaluate the impact of metabolic and transporter inhibition on investigational drugs. The combination is used to gauge the changes in relative bioavailability, pharmacokinetics, safety, and tolerability of BI 691751 when its metabolism and transport are inhibited by itraconazole.

Other names
BI 691751BI691751BI-691751itraconazole
02

Targets

ABCB1 (P-glycoprotein)CYP3A4 (Cytochrome P450 3A4)LTA4H (Leukotriene A4 hydrolase)

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